cholestyramine (Rx)

Brand and Other Names:Prevalite, Questran, more...Questran Light, LoCholest
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

packet

  • 4g

powder for oral suspension

  • 4g/dose (231g)
  • 4g/dose (378g)
  • 4g/dose (210g)

Hyperlipidemia

4 g PO q12-24hr; increase gradually over ≥1 month intervals

Maintenance: 8-16 g/day PO divided q12hr; not to exceed 24 g/day

Overdose: Symptoms include gastrointestinal (GI) obstruction; treatment is supportive

Dosing Modifications

Renal impairment: Supplemental doses not necessary with peritoneal dialysis (PD) or hemodialysis (HD)

Administration

Always mix with fluids or food

Take before or with meals

Dosage Forms & Strengths

powder for oral suspension

  • 4g resin/5g powder
  • 4g resin/5.5g powder
  • 4g resin/5.7g powder
  • 4g resin/6.4g powder
  • 4g resin/9g powder

Hyperlipidemia

240 mg/kg/day PO divided q8-12hr; generally not to exceed 8 g/day  

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Interactions

Interaction Checker

and cholestyramine

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            Contraindicated (1)

            • mycophenolate

              cholestyramine decreases levels of mycophenolate by inhibition of GI absorption. Applies only to oral form of both agents. Contraindicated. Cholestyramine binds bile acids and reduces mycophenolic acid exposure.

            Serious - Use Alternative (1)

            • warfarin

              cholestyramine decreases effects of warfarin by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Cholestyramine and vitamin K antagonists should be administered 3-4 hr apart and monitor patients closely for reduced vitamin K antagonist effects.

            Monitor Closely (64)

            • amiodarone

              cholestyramine decreases levels of amiodarone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • atorvastatin

              cholestyramine decreases levels of atorvastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • bendroflumethiazide

              cholestyramine decreases levels of bendroflumethiazide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • beta carotene

              cholestyramine decreases levels of beta carotene by drug binding in GI tract. Use Caution/Monitor.

            • budesonide

              cholestyramine decreases levels of budesonide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • calcifediol

              cholestyramine will decrease the level or effect of calcifediol by drug binding in GI tract. Modify Therapy/Monitor Closely. Dose adjustment of calcifediol may be required, and serum total 25-hydroxyvitamin D, intact PTH, and serum calcium concentrations should be monitored closely if cholestyramine is initiated or discontinued.

            • chlorothiazide

              cholestyramine decreases levels of chlorothiazide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • chlorthalidone

              cholestyramine decreases levels of chlorthalidone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • cholic acid

              cholestyramine will decrease the level or effect of cholic acid by drug binding in GI tract. Use Caution/Monitor. Take cholic acid at least 1 hr before or 4-6 hr (or as great an interval as possible) after a bile acid binding resin.

            • cortisone

              cholestyramine decreases levels of cortisone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • deferasirox

              cholestyramine decreases levels of deferasirox by Other (see comment). Use Caution/Monitor. Comment: Avoid concomitant use of cholestyramine with deferasirox. If co-administration is required then consider increasing initial dose of deferasirox to 30 mg/kg and monitor serum ferritin levels and clinical response.

            • deflazacort

              cholestyramine decreases levels of deflazacort by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • demeclocycline

              cholestyramine decreases levels of demeclocycline by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • dexamethasone

              cholestyramine decreases levels of dexamethasone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • diclofenac

              cholestyramine decreases levels of diclofenac by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • digoxin

              cholestyramine decreases levels of digoxin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • doxercalciferol

              cholestyramine decreases levels of doxercalciferol by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. (Vitamin D analog).

            • doxycycline

              cholestyramine decreases levels of doxycycline by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • ezetimibe

              cholestyramine decreases levels of ezetimibe by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Separate by 2-4 hours.

            • fenofibrate

              cholestyramine decreases levels of fenofibrate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • fenofibrate micronized

              cholestyramine decreases levels of fenofibrate micronized by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • fenofibric acid

              cholestyramine decreases levels of fenofibric acid by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • fludrocortisone

              cholestyramine decreases levels of fludrocortisone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • fluvastatin

              cholestyramine decreases levels of fluvastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • furosemide

              cholestyramine decreases levels of furosemide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • gemfibrozil

              cholestyramine decreases levels of gemfibrozil by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • hydrochlorothiazide

              cholestyramine decreases levels of hydrochlorothiazide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • hydrocortisone

              cholestyramine decreases levels of hydrocortisone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • imipramine

              cholestyramine decreases levels of imipramine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • indapamide

              cholestyramine decreases levels of indapamide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • leflunomide

              cholestyramine decreases levels of leflunomide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • levothyroxine

              cholestyramine decreases levels of levothyroxine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • liothyronine

              cholestyramine decreases levels of liothyronine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • lomitapide

              cholestyramine decreases levels of lomitapide by drug binding in GI tract. Use Caution/Monitor. Separate lomitapide and administration of bile acid sequestrants by at least 4 hours; bile acid sequestrants can interfere with the absorption of oral medications.

            • lovastatin

              cholestyramine decreases levels of lovastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • meloxicam

              cholestyramine decreases levels of meloxicam by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • methotrexate

              cholestyramine decreases levels of methotrexate by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. To minimize drug interactions, administer other drugs at least 1 hour before or at least 4-6 hours after the administration of cholestyramine.

            • methyclothiazide

              cholestyramine decreases levels of methyclothiazide by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • methylprednisolone

              cholestyramine decreases levels of methylprednisolone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • metolazone

              cholestyramine decreases levels of metolazone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • metronidazole

              cholestyramine decreases levels of metronidazole by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • minocycline

              cholestyramine decreases levels of minocycline by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • niacin

              cholestyramine decreases levels of niacin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • obeticholic acid

              cholestyramine will decrease the level or effect of obeticholic acid by drug binding in GI tract. Modify Therapy/Monitor Closely. Administer obeticholic acid at least 4 hr before or 4 hr after taking a bile acid binding resins.

            • odevixibat

              cholestyramine will decrease the level or effect of odevixibat by drug binding in GI tract. Modify Therapy/Monitor Closely. Administer bile acid sequestrants 4 hr before or after odevixibat.

            • omadacycline

              cholestyramine will decrease the level or effect of omadacycline by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Monitor for decreased effects of tetracyclines if coadministered with a bile acid sequestrant. Separate doses 2 or more hours if these agents are used concomitantly.

            • oxytetracycline

              cholestyramine decreases levels of oxytetracycline by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • paricalcitol

              cholestyramine decreases levels of paricalcitol by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. (Vitamin D analog).

            • piroxicam

              cholestyramine decreases levels of piroxicam by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • pitavastatin

              cholestyramine decreases levels of pitavastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • pravastatin

              cholestyramine decreases levels of pravastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • prednisolone

              cholestyramine decreases levels of prednisolone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • prednisone

              cholestyramine decreases levels of prednisone by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • raloxifene

              cholestyramine decreases levels of raloxifene by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • rosuvastatin

              cholestyramine decreases levels of rosuvastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • sarecycline

              cholestyramine will decrease the level or effect of sarecycline by inhibition of GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Monitor for decreased effects of tetracyclines if coadministered with a bile acid sequestrant. Separate doses by 2 or more hours if coadministered.

            • simvastatin

              cholestyramine decreases levels of simvastatin by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • spironolactone

              cholestyramine, spironolactone. unspecified interaction mechanism. Use Caution/Monitor. Hyperkalemic metabolic acidosis reported when coadministered.

            • tetracycline

              cholestyramine decreases levels of tetracycline by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • thyroid desiccated

              cholestyramine decreases levels of thyroid desiccated by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • tinidazole

              cholestyramine will decrease the level or effect of tinidazole by Other (see comment). Use Caution/Monitor. Coadministration of cholestyramine with tinidazole may decrease absorption of tinidazole. Advise to separate dosing regimens for cholestyramine and tinidazole to minimize any potential effect on the oral bioavailability of tinidazole.

            • triamcinolone acetonide injectable suspension

              cholestyramine decreases levels of triamcinolone acetonide injectable suspension by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • valproic acid

              cholestyramine decreases levels of valproic acid by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor.

            • vitamin D

              cholestyramine will decrease the level or effect of vitamin D by Other (see comment). Use Caution/Monitor. Bile acid sequestrants may decrease the absorption of fat-soluble vitamins. Administer vitamin supplementation at least 4 hours prior to cholestyramine.

            Minor (7)

            • acetaminophen

              cholestyramine decreases levels of acetaminophen by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

            • acetaminophen IV

              cholestyramine decreases levels of acetaminophen IV by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

            • acetaminophen rectal

              cholestyramine decreases levels of acetaminophen rectal by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

            • chenodiol

              cholestyramine decreases levels of chenodiol by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

            • ursodiol

              cholestyramine decreases effects of ursodiol by pharmacodynamic antagonism. Minor/Significance Unknown.

            • vitamin A

              cholestyramine decreases levels of vitamin A by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown. (Vitamin A).

            • vitamin K1 (phytonadione)

              cholestyramine decreases levels of vitamin K1 (phytonadione) by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown. (Vitamin K).

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            Adverse Effects

            Frequency Not Defined

            Belching

            Constipation

            Dental erosion

            Diarrhea

            Duodenal ulcer bleeding

            Flatulence

            Gallstones

            Heartburn

            Hypoprothrombinemia

            Malabsorption of fat-soluble vitamins

            Nausea and vomiting

            Pancreatitis

            Perianal irritation

            Rectal pain

            Steatorrhea

            Stomach pain

            Weight gain or loss

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            Warnings

            Contraindications

            Hypersensitivity to bile-sequestering resins

            Complete biliary obstruction

            Cautions

            Use with caution in renal impairment

            Volume depletion

            Concomitant spironolactone therapy

            Not for use with baseline fasting triglyceride levels ≥300 mg/dL or type III hyperlipoproteinemia; use with caution in patients with triglyceride levels 250-299 mg/dL; perform fasting lipid panel in 4-6weeks after initiation; discontinue use if triglycerides are >400 mg/dL; secondary causes of hyperlipidemia must be ruled out before therapy is initiated

            Not to be used as monotherapy in hypertriglyceridemia

            With prolonged use, increased risk of bleeding because of hypoprothrombinemia from vitamin K deficiency

            May interfere with fat absorption and decrease absorption of fat-soluble vitamins (A, D, E, K)

            May exacerbate preexisting constipation (initiate therapy at lower dosage in patients with history of constipation)

            Special care must be taken to avoid constipation in patients with symptomatic coronary heart disease

            Always mix with water or fluids; never ingest dry powder

            Some formulations contain phenylalanine

            Because of large quantities of chloride ion released from resin (which may lead to hyperchloremic acidosis and increase urinary calcium excretion on prolonged use), it may be advisable to reduce chloride intake

            Take other drugs at least 1 hour before or 4-6 hours after taking cholestyramine to minimize possible interference with absorption

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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Drug does not enter breast milk; use with caution because of potential vitamin loss in mother

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            Forms complex with bile acids that is not absorbed through intestine; inhibits enterohepatic reuptake of intestinal bile salts, and this, in turn, increases fecal loss of bile salt-bound LDL and consequently reduces serum cholesterol in patients with primary hypercholesterolemia

            Absorption

            Not absorbed

            Peak effect: 21 days

            Metabolism

            Not metabolized

            Elimination

            Excretion: Feces (insoluble complex with bile acids)

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
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            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.